1,2,4-triazole derivatives as histamine h.sub.2- antagonists

Details 1,2,4-triazole derivatives as histamine h.sub.2- antagonists 1,2,4-triazole derivatives as histamine h.sub.2- antagonists

C - Chemistry, Metallurgy

07

D

260/237.1, 260/3

C07D 249/14 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01)

Patent

CA 1188689

ABSTRACT OF THE DISCLOSURE This invention disclosure novel heterocyclic derivatives, the processes for their production and pharmeceutical compositions containing same. In particu1ar, it disclosures compounds of the general formula (I) Image and physiologically acceptab1e salts, hydrates and bio- precursors thereof, in which Rl and R2 which may be the same or diffcrent, each represent hydrogen, Cl-10 alkyl, cycloalkyl, alkenyl, aralkyl, trifluoroalkyl, or alkyl, substituted by hydroxy, alkoxy, amino, alkylamino or dialkylamino, or Rl and R2 may together with the nitroqen atom to which they are attached form a 5 to 10 membered ring which may be sat- urated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more Cl-3 alkyl groups or a hydroxy group and/or may contain another heteroatom which i8 oxygen or sulphur; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms Q represent3 a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5- positions, the furan ring option- ally bearing a further substituent R6 adjacent to the group RlR2N-Alk-, or Q represents a benzene ring in which incorp- oration into the reet of the molecule is through bonds at the 1- and 3- or 1- and 4- positions; R6 represents halogen or Cl-4 alkyl which may be substituted by hydroxy or Cl-4 alkoxy; X represents -CH2-, -O-,-S- or -N- where Image R5 represents hydrogen or methyl; n represents zero,1 or 2, m represents 2,3 or 4; R3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxy- alkyl with at least two carbon atoms, alkoxyalkyl or aryl; and R4 represents hydrogen, alkyl, alkenyl, aryl, aralkyl, hydroxyalkyl, acyloxyalkyl, alkoxyalkyl, aryl- oxyalkyl, aralkyloxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxy, alkoxy, alkylthio or halogen. These compounds show pharmacological activity as selective histamine H2-antagonists.

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